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Cat. No.: HY-151248

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HDAC2-IN-1

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC₅₀ of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC₅₀s of 1.61 μM and 0.98 μM, respectively.

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CAS No.: 2919691-32-8
Formule: C₂₂H₂₃ClN₄OS
Masse moléculaire:426.96

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

HDAC2-IN-1 Chemical Structure

CAS No.: 2919691-32-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC₅₀ of 0.5 μM^[1]. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC₅₀s of 1.61 μM and 0.98 μM, respectively^[1].

IC₅₀ & Target^[1]

HDAC2

0.5 μM (IC₅₀)

HDAC8

0.98 μM (IC₅₀)

HDAC1

1.61 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform HDAC :

In Vitro

HDAC2-IN-1 (Compound 17) (3 and 10 μM; 48 h) increases histone H4K12 and H3K9 acetylation levels in SKNSH cells in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

HDAC2-IN-1 (Compound 17) (30 or 100 mg/kg; p.o.; once) shows good plasma and brain exposure, and shows promising brain penetration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6 mice^[1]
Dosage:

30 or 100 mg/kg
Administration:

Oral administration (Pharmacokinetic Analysis)
Result:

Showed good plasma and brain exposure, also showed promising brain penetration, K_p,uu = 0.36. Significantly increased histone H4K12 acetylation in mouse brain 4 h after oral dosing at 100 mg/kg.

Chemical Information

CAS No. 2919691-32-8
Masse moléculaire 426.96
Formule C₂₂H₂₃ClN₄OS
SMILES

ClC1=CC([C@@H]2C[C@H](C(N3CCN(CC3)C4=NC=CC5=C4SC=C5)=O)NC2)=CC=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Tamanini E, et al. Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor. ACS Medicinal Chemistry Letters, 2022.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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HDAC2-IN-1

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

HDAC2-IN-1 Related Classifications

HY-151248 Related Classifications